Organic Cation Transporter–Mediated Clearance of Cardiovascular Drugs

There exist a number of mechanisms to clear xenobiotics from human circulation. For cationic drugs, clearance is performed by human organic cation transporters 1 and 2 (hOCT1 and hOCT2), which are expressed in the liver and kidney, respectively. Given the prevalence of patients taking cardiovascular drugs, the present review focuses on the elimination of circulating cardiovascular drugs by organic cation transporters (OCTs). A significant number of cardiovascular drugs compete for transport by OCT1 or OCT2, introducing the potential to alter the pharmacokinetic profile of other concomitantly administered medications. The OCT system thereby represents an important site of drug-drug interactions.